CN110573508B - 稠合咪唑并-哌啶jak抑制剂化合物 - Google Patents

稠合咪唑并-哌啶jak抑制剂化合物 Download PDF

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CN110573508B
CN110573508B CN201880028413.7A CN201880028413A CN110573508B CN 110573508 B CN110573508 B CN 110573508B CN 201880028413 A CN201880028413 A CN 201880028413A CN 110573508 B CN110573508 B CN 110573508B
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crystalline form
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CN110573508A (zh
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P·R·法特里
姜岚
R·M·麦金内尔
V·R·萨兰迪
张�浩
M·达布罗斯
J·恩泽雷姆
N·本杰明
M·A·克莱因舍尔克
G·D·克拉泰尔
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Theravance Biopharma R&D IP LLC
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0048Eye, e.g. artificial tears
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/10Dispersions; Emulsions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/08Bronchodilators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Dispersion Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
CN201880028413.7A 2017-05-01 2018-04-30 稠合咪唑并-哌啶jak抑制剂化合物 Active CN110573508B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762492574P 2017-05-01 2017-05-01
US62/492,574 2017-05-01
PCT/US2018/030148 WO2018204238A1 (en) 2017-05-01 2018-04-30 Fused imidazo-piperidine jak inhibitor compound

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CN110573508A CN110573508A (zh) 2019-12-13
CN110573508B true CN110573508B (zh) 2022-07-05

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US (3) US10493077B2 (pl)
EP (1) EP3601283B1 (pl)
JP (1) JP7098656B2 (pl)
KR (1) KR102550225B1 (pl)
CN (1) CN110573508B (pl)
AR (1) AR111495A1 (pl)
AU (1) AU2018261593B2 (pl)
BR (1) BR112019022648A2 (pl)
CA (1) CA3056283A1 (pl)
CL (1) CL2019003086A1 (pl)
CO (1) CO2019011809A2 (pl)
CY (1) CY1125051T1 (pl)
DK (1) DK3601283T3 (pl)
EA (1) EA201992601A1 (pl)
ES (1) ES2908756T3 (pl)
HR (1) HRP20220330T1 (pl)
IL (1) IL270231B2 (pl)
LT (1) LT3601283T (pl)
MA (1) MA47970B1 (pl)
MD (1) MD3601283T2 (pl)
MX (1) MX2019012942A (pl)
NZ (1) NZ757570A (pl)
PH (1) PH12019502264A1 (pl)
PL (1) PL3601283T3 (pl)
PT (1) PT3601283T (pl)
RS (1) RS62995B1 (pl)
SG (1) SG11201908604YA (pl)
SI (1) SI3601283T1 (pl)
TW (1) TWI760486B (pl)
UA (1) UA124478C2 (pl)
WO (1) WO2018204238A1 (pl)

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EP3371186A1 (en) 2015-11-03 2018-09-12 Theravance Biopharma R&D IP, LLC Jak kinase inhibitor compounds for treatment of respiratory disease
SG11201907544VA (en) 2017-03-09 2019-09-27 Theravance Biopharma R&D Ip Llc Jak inhibitors containing a 4-membered heterocyclic amide
US10406148B2 (en) 2017-05-01 2019-09-10 Theravance Biopharma R&D Ip, Llc Methods of treatment using a JAK inhibitor compound
AR111495A1 (es) 2017-05-01 2019-07-17 Theravance Biopharma R&D Ip Llc Compuestos de imidazo-piperidina fusionada como inhibidores de jak
MA53229A (fr) 2018-09-04 2022-05-11 Theravance Biopharma R&D Ip Llc Amides de diméthyl amino azétidine utilisés en tant qu'inhibiteurs de jak
AR116116A1 (es) 2018-09-04 2021-03-31 Theravance Biopharma R&D Ip Llc Proceso para elaborar inhibidores de jak e intermediarios de los mismos
MX2021002484A (es) 2018-09-04 2021-05-12 Theravance Biopharma R&D Ip Llc Amidas heterociclicas de 5 a 7 miembros como inhibidores de jak.
US10968222B2 (en) 2018-10-29 2021-04-06 Theravance Biopharma R&D Ip, Llc 2-azabicyclo hexane JAK inhibitor compound
JP2022517316A (ja) 2019-01-11 2022-03-08 ネイジス ファーマシューティカルズ インコーポレイテッド ロイコトリエン合成阻害剤
BR112021016751B8 (pt) 2019-02-25 2023-11-21 Henan Medinno Pharmaceutical Tech Co Ltd Compostos, composições farmacêuticas e usos dos compostos
MX2021010545A (es) 2019-03-05 2021-11-17 Incyte Corp Inhibidores de la vía de cinasa janus 1 (jak1) para el tratamiento de la disfunción crónica del aloinjerto pulmonar.
CN114364798A (zh) 2019-03-21 2022-04-15 欧恩科斯欧公司 用于治疗癌症的Dbait分子与激酶抑制剂的组合
KR20220098759A (ko) 2019-11-08 2022-07-12 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) 키나제 억제제에 대해 내성을 획득한 암의 치료 방법
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
TW202144343A (zh) 2020-03-02 2021-12-01 美商施萬生物製藥研發 Ip有限責任公司 Jak抑制劑化合物之結晶水合物
WO2021185305A1 (zh) * 2020-03-18 2021-09-23 四川海思科制药有限公司 一种吲唑衍生物及其在医药上的应用
CN111620868B (zh) * 2020-05-28 2021-08-31 爱斯特(成都)生物制药股份有限公司 一种1H-吡唑并[3,4-b]吡啶-3-甲醛的制备方法
WO2022272020A1 (en) * 2021-06-25 2022-12-29 Theravance Biopharma R&D Ip, Llc Imidazolo indazole compounds as jak inhibitors
CN114181055A (zh) * 2021-12-21 2022-03-15 苏州楚凯药业有限公司 1-苄氧基-4-溴-5-乙基-2-氟苯的制备方法

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KR102550225B1 (ko) 2023-07-03
MA47970B1 (fr) 2022-03-31
NZ757570A (en) 2021-07-30
EP3601283A1 (en) 2020-02-05
WO2018204238A1 (en) 2018-11-08
US11160810B2 (en) 2021-11-02
TW201841914A (zh) 2018-12-01
SG11201908604YA (en) 2019-10-30
CL2019003086A1 (es) 2020-01-24
MD3601283T2 (ro) 2022-05-31
PT3601283T (pt) 2022-02-10
CY1125051T1 (el) 2024-02-16
IL270231B2 (en) 2023-08-01
MX2019012942A (es) 2019-12-16
IL270231B1 (en) 2023-04-01
CN110573508A (zh) 2019-12-13
PL3601283T3 (pl) 2022-05-02
AU2018261593A1 (en) 2019-10-17
UA124478C2 (uk) 2021-09-22
CA3056283A1 (en) 2018-11-08
JP2020518581A (ja) 2020-06-25
CO2019011809A2 (es) 2020-01-17
DK3601283T3 (da) 2022-04-04
US20200046719A1 (en) 2020-02-13
US20220008428A1 (en) 2022-01-13
TWI760486B (zh) 2022-04-11
HRP20220330T1 (hr) 2022-05-13
US10493077B2 (en) 2019-12-03
SI3601283T1 (sl) 2022-04-29
AU2018261593B2 (en) 2021-08-26
LT3601283T (lt) 2022-02-25
IL270231A (pl) 2019-12-31
RS62995B1 (sr) 2022-03-31
US20180311255A1 (en) 2018-11-01
EP3601283B1 (en) 2021-12-29
JP7098656B2 (ja) 2022-07-11
ES2908756T3 (es) 2022-05-03
AR111495A1 (es) 2019-07-17
KR20190142389A (ko) 2019-12-26
EA201992601A1 (ru) 2020-03-03
BR112019022648A2 (pt) 2020-05-19
PH12019502264A1 (en) 2020-09-21

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